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Tamatinib besylate (R406)

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Tamatinib besylate (R406)
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Size Price Stock
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1g$2430Check With Us

Cat #: V0583 CAS #: 841290-81-1 Purity ≥ 98%

Description: Tamatinib besylate (formerly R-406 besylate; prodrug of R 406) is a novel, potent and ATP-competitive inhibitor of spleen tyrosine kinase/Syk with potential anti-inflammatory activity.

References: Sylvia Braselmann, et al. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008.

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Molecular Weight (MW)628.63
Molecular FormulaC22H23FN6O5.C6H6O3S
CAS No.841290-81-1
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 126 mg/mL (200.4 mM)r
Water: <1 mg/mLr
Ethanol: 8 mg/mL (12.7 mM)
Solubility In Vivo30% PEG400+0.5% Tween80+5% Propylene glycol: 30 mg/mL
SMILES CodeCC1(C(=O)NC2=C(O1)C=CC(=N2)NC3=NC(=NC=C3F)NC4=CC(=C(C(=C4)OC)OC)OC)C.C1=CC=C(C=C1)S(=O)(=O)O
SynonymsR406 benzenesulfonate; R-406 benzenesulfonate; R-406 besylate; R406; R-406; R 406; R 406 besylate; R406 besylate; R406 benzenesulfonate; Tamatinib,
ProtocolIn VitroR406 inhibits phosphorylation of Syk substrate LAT in mast cells and BLNK/SLP65 in B cells. R406 inhibits Huh7 hepatocyte, A549 epithelial, and H1299 lung cancer lines with EC50s of 15.1, 2.9 and 6.3 µM, respectively. R406 inhibits adenosine A3 receptor (IC50=0.081 µM), adenosine transporter (IC50=1.84 µM), and monoamine transporter (IC50=2.74 µM).
In VivoR406 (5 and 10 mg/kg) shows efficacy in the amelioration of the Arthus reaction and in reducing clinical symptoms in the collagen antibody-induced arthritis (CAIA) and K/BxN models of rheumatoid arthritis (RA). Immune complex (IC)-mediated inflammation is reduced by inhibition of Fc receptor signaling with R406.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.5908 mL7.9538 mL15.9076 mL31.8152 mL
5mM0.3182 mL1.5908 mL3.1815 mL6.3630 mL
10mM0.1591 mL0.7954 mL1.5908 mL3.1815 mL
20mM0.0795 mL0.3977 mL0.7954 mL1.5908 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
  • (2) Be sure to add the solvent(s) in order.